Efonidipine

Catalog No.S4977 Batch:S497702

Technical Data

Formula	C₃₄H₃₈N₃O₇P
Molecular Weight	631.66	CAS No.	111011-63-3
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (158.31 mM)
		Ethanol	6 mg/mL (9.49 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

Efonidipine (NZ-105) is an L- and T-type calcium channel blocker leading to vasodilation and decreased automaticity of the heart. It also suppresses aldosterone secretion from the adrenal.

Targets

T-type calcium channel ^[2]

In vitro

Although efonidipine is not a specific T-type calcium channe (TTCC) blocker as it could also block L-type calcium channe (LTCC), its efficacy in blocking TTCC is much greater than that of LTCC^[1]. Efonidipine exerts an inhibitory effect on aldosterone synthesis and secretion in a human adrenocortical cell line (H295R), an effect that is mediated, at least in part, by suppression of 11-β-hydroxylase and aldosterone synthase expression. Efonidipine also suppresses both Ang II- and K+-induced aldosterone secretion, but it blocks the latter at much lower concentrations than the former^[2].

In vivo

Efonidipine could provide broader beneficial effects including the heart, liver, and plasma, and antioxidant in iron-overload condition in both WT(muβ^+⁄+) and HT(muβ^{th-3 ⁄+},) mice^[1].

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines The NCI-H295R human adrenocortical cell line (H295) Concentrations 0.3 μM and 3 μM Incubation Time 24 h Method H295R cells are plated to a density of 0.2 × 10⁶ in 6-well plates and incubated for 48 hours, after which the medium is replaced with low-serum medium containing 0.2% UltroserSF, and the cells are then treated with Ang II (100 nmol/L) or KCl (10 mmol/L) with or without the indicated concentration of Ca2+ channel blocker for 24 hours. The cells are then harvested, and the total cellular RNA is extracted using the isothiocyanate-acid phenol chloroform method. After quantifying the extracted RNA based on absorbance at 260 nm, 500-ng aliquots are reverse transcribed.
Animal Study:^{^[1]}	Animal Models adult C57/BL6 mice (3-6 months old, heterozygous β^KO type) with FE diet (0.2% ferrocene w⁄w) Dosages 4 mg⁄kg Administration i.p.

Cell Assay:^{^[2]}

Cell lines
The NCI-H295R human adrenocortical cell line (H295)
Concentrations
0.3 μM and 3 μM
Incubation Time
24 h
Method
H295R cells are plated to a density of 0.2 × 10⁶ in 6-well plates and incubated for 48 hours, after which the medium is replaced with low-serum medium containing 0.2% UltroserSF, and the cells are then treated with Ang II (100 nmol/L) or KCl (10 mmol/L) with or without the indicated concentration of Ca2+ channel blocker for 24 hours. The cells are then harvested, and the total cellular RNA is extracted using the isothiocyanate-acid phenol chloroform method. After quantifying the extracted RNA based on absorbance at 260 nm, 500-ng aliquots are reverse transcribed.

Animal Study:^{^[1]}

Animal Models
adult C57/BL6 mice (3-6 months old, heterozygous β^KO type) with FE diet (0.2% ferrocene w⁄w)
Dosages
4 mg⁄kg
Administration
i.p.

References

Selleck's Efonidipine has been cited by 1 publication

Efonidipine Inhibits JNK and NF-κB Pathway to Attenuate Inflammation and Cell Migration Induced by Lipopolysaccharide in Microglial Cells [ Biomol Ther (Seoul), 2022, 30(5):455-464]	PubMed: 35993250

Efonidipine Inhibits JNK and NF-κB Pathway to Attenuate Inflammation and Cell Migration Induced by Lipopolysaccharide in Microglial Cells [ Biomol Ther (Seoul), 2022, 30(5):455-464]

PubMed: 35993250

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.